Active substanceBrimonidineBrimonidine
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  • Dosage form: & nbspeye drops
    Composition:

    1 ml contains:

    Active substance: Brimonidine tartrate 2.0 mg.

    Excipients: Benzalkonium chloride (in terms of 100% substance) - 0.052 mg, polyvinyl alcohol-14.00 mg, sodium chloride - 6.90 mg, sodium citrate dihydrate - 4.70 mg, citric acid monohydrate 0.48 mg, 1 M solution of hydrochloric acid or 1 M sodium hydroxide solution to pH 6.45, water purified to 1 ml.

    Description:A clear solution of a greenish-yellow color.

    Pharmacotherapeutic group:Antiglaucoma means - alpha2-adrenomimetic selective
    ATX: & nbsp

    S.01.E.A   Sympathomimetics for the treatment of glaucoma

    S.01.E.A.05   Brimonidine

    Pharmacodynamics:

    Brimonidine is a selective alpha2-adrenergic receptor agonist. When instillation 0.2% brimonidine solution decrease in intraocular pressure is 10-12 mm Hg, the maximum decrease in intraocular pressure is achieved after 2 hours, the duration of action is 12 hours. Brimonidine has a double mechanism of action, it can lower intraocular pressure by decreasing the synthesis of intraocular fluid and enhancing uveoscleral outflow.

    Pharmacokinetics:

    After applying a 0.2% solution of eye drops of brimonidine twice a day for 10 days, the average value of the maximum concentration (CmOh) in blood plasma remains low (an average of 0.06 ng / ml).

    When instillation of eye drops, the maximum concentration of the drug in the blood plasma is achieved after 0.5-2.5 hours, half-life (T1/2) of the drug after topical application on average is 2 hours.

    The connection with plasma proteins during local application is 29%. Brimonidine reversibly binds to melanin. The concentrations of brimonidine in the iris, ciliary body and retina after two weeks of instillation into the eyes were 3-17 times higher than these values ​​after instillation of one dose of the drug. Systemic absorption of brimonidine in local application is slowed down.

    The drug is metabolized primarily in the liver. Are deduced brimonidine and its metabolites by the kidneys.

    Indications:Open angle glaucoma, ophthalmic hypertension (in monotherapy and in combination with other drugs that reduce intraocular pressure).
    Contraindications:

    - Hypersensitivity to brimonidine or any of the excipients.

    - Simultaneous reception with monoamine oxidase (MAO) inhibitors and tricyclic or tetracyclic antidepressants (including myanserin).

    - Children under 2 years old (safety and efficacy of the drug for this age group are not established).

    - The period of breastfeeding.

    Carefully:

    In patients with renal insufficiency (creatinine clearance below 40 ml / min) and liver failure.

    In patients with orthostatic hypotension, heart failure and cerebral circulatory insufficiency, depression, Reynaud's syndrome, obliterative thromboangiitis, Luxfen® can increase the severity of the course of diseases caused by vascular insufficiency.

    In patients who are simultaneously taking therapy with antihypertensive drugs and / or cardiac glycosides.

    Children aged 2 to 18 years (safety and efficacy not established). During the period of treatment, careful monitoring of the condition of patients aged 2 to 7 years (especially with a body weight of up to 20 kg) is necessary because of the high incidence and severity of drowsiness.

    The use of the drug in children younger than 12 years is not recommended.

    When developing allergic reactions to the drug - it is necessary to stop treatment and consult a doctor.

    It is possible to increase intraocular pressure in case of delayed hypersensitivity reactions (see section "Side effect"). Contained in the preparation of preservative (benzalkonium chloride) can cause eye irritation.

    Pregnancy and lactation:The safety of the use of this drug during pregnancy in humans is not defined. In animal studies, the local use of brimonidine did not lead to a disruption of intrauterine development. The use of brimonidine in pregnancy is allowed only in cases where the expected benefit to the mother exceeds the potential risk to the fetus. There is no precise data on the penetration of brimonidine in breast milk in topical application. However, the risk can not be ruled out completely. The use of the drug during breastfeeding is contraindicated (see section "Contraindications").
    Dosing and Administration:

    Locally.

    In the conjunctival sac of the affected eye, 1 drop 2 times a day with an interval between administrations of 12 hours.

    The duration of treatment is determined by the doctor.

    In order to reduce the possible systemic absorption of the drug, it is recommended to squeeze the lacrimal sac at the inner corner of the eye (closing the lacrimal point) for one minute. This method should be performed immediately after instillation of each drop.

    If it is necessary to use two or more ophthalmic preparations, different preparations should be instilled at intervals of 5-15 minutes.

    Patients with impaired renal and hepatic function

    The use of Luxfen® in patients with hepatic or renal dysfunction has not been studied, caution should be exercised in the treatment of such patients (see "With caution").

    Elderly patients

    In elderly patients, there were no differences in safety or efficacy compared with other adult patients. FROMmOh and T1/2 Brimonidine were similar in the elderly (65 years and older) and younger adults, which demonstrates the absence of a significant effect of age on systemic absorption and on the excretion of brimonidine. No dose adjustment is required in the treatment of elderly patients.

    Application the children

    Brimonidine is contraindicated in children under 2 years of age (see p.section "Contraindications").

    In children 2 to 7 years of age, 0.2% of brimonidine may cause drowsiness, which may lead to discontinuation of treatment. Careful monitoring of the patient's condition should be made, due to the high frequency of cases of drowsiness.

    The incidence of drowsiness may decrease with age, but is more determined by body weight: in children <20 kg, somnolence may be more frequent than in children> 20 kg (see "With caution").

    Side effects:The most common undesirable reactions from the side of the organ of vision are allergic conjunctivitis, conjunctival hyperemia, itching of the eye mucosa and eyelid skin. Most of the undesirable reactions had a quick-passing nature and mild severity (do not require discontinuation of treatment). According to clinical studies, symptoms of allergic reactions from the eyes were observed in 12.7% of cases (being the reason for the termination of treatment in 11.5% of cases), while in most patients they manifested themselves in 3-6 months of application of the drug.

    The frequency of undesirable effects was classified as follows: very often (≥ 1/10), often (from ≥ 1/100 to <1/10), infrequently (from ≥ 1/1 000 to <1/100),rarely (from ≥ 1/10 000 to <1/1 000), very rarely (<1/10 000), the frequency of occurrence is unknown (it is impossible to estimate based on available data).

    From the side of the organ of vision:

    Often - congestion hyperemia, burning sensation, itchy eyelid skin and eye mucosa, foreign body sensation, impaired vision, allergic blepharitis, allergic blepharoconjunctivitis, allergic conjunctivitis, follicular conjunctivitis.

    Often - hyperemia and edema of the eyelids, blepharitis, conjunctival edema and mucous discharge from the eyes, conjunctival hemorrhage, conjunctivitis, retinal lacrimation, epiphora, eye pain and lacrimation, conjunctival eye folliculosis, local allergic reactions of the eye mucosa (including keratoconjunctivitis), cataracts , keratitis, lesions of the eyelids, photosensitivity, superficial spotted keratopathy, loss of the visual field, functional damage of the vitreous humor, vitreous hemorrhage, floating opacities in the vitreous humus barely and reduced visual acuity, photophobia, erosion and opacity of the cornea, dryness and irritation of the mucous membrane of the eye surface, blanching of the conjunctiva.

    Infrequently - barley.

    Rarely - Irit, miosis.

    From the central nervous system:

    Often - headache, drowsiness.

    Often - dizziness, a violation of taste.

    Infrequently - Depression.

    Rarely - fainting, insomnia.

    From the cardiovascular system:

    Infrequently - palpitations / arrhythmias (including bradycardia and tachycardia).

    Very rarely - increase or decrease in blood pressure.

    On the part of the respiratory system:

    Often - bronchitis, pharyngitis, cough, shortness of breath.

    Infrequently dryness of the nasal mucosa.

    Rarely - shortness of breath.

    From the gastrointestinal tract:

    Often - dryness of the oral mucosa.

    Often - gastrointestinal disorders - dyspepsia.

    From the skin and subcutaneous fat:

    Often - rash.

    Infectious and parasitic diseases:

    Often - flu-like syndrome, infectious disease (chills and respiratory infection), rhinitis, sinusitis, incl. infectious.

    From the immune system:

    Infrequently - Systemic allergic reactions.

    Laboratory indicators:

    Often - hypercholesterolemia.

    Others:

    Often - fatigue.

    Often - asthenia.

    Children noted: apnea, bradycardia, lowering blood pressure, hypothermia, muscle hypotension, pallor, drowsiness, decreased attention (see section "With caution").

    Post-marketing application of 2 mg / ml eye drops of brimonidine revealed unwanted reactions (indicated below), the source of which was spontaneous reports with an unknown population size, therefore indicate the frequency of their occurrence is not possible:

    from the side of the organ of vision: iridocyclitis (anterior uveitis);

    from the skin and subcutaneous fat: allergic reactions from the skin, including erythema, face swelling, itching, rash and vasodilation of the skin of the eyelid;

    from the gastrointestinal tract: nausea.

    Overdose:Overdose in topical application

    Symptoms of overdose with topical application of the drug are presented previously noted undesirable reactions.

    Overdose with a random intake of the drug inside (adult patients)

    Reports of cases of overdose in adults are quite small.

    The following symptoms are possible: depression of the central nervous system, drowsiness, oppression and loss of consciousness, hypotension, bradycardia,decrease in body temperature, cyanosis of the skin, apnea, asthenia, vomiting, convulsions, arrhythmia, miosis.

    Treatment overdose when taking the drug inside includes supportive and symptomatic therapy, it is necessary to maintain the patency of the airways.

    Overdose in children

    An overdose of brimonidine (as an additional therapy for congenital glaucoma or accidental ingestion) was observed in young children (2-7 years).

    Symptoms: loss of consciousness, inhibition, drowsiness, hypotension, hypotension, bradycardia, hypothermia, cyanosis, pallor, respiratory depression and apnea.

    Treatment: maintenance and symptomatic therapy, control of airway patency, intensive therapy with intubation may be necessary.

    Interaction:

    Studies on the study of drug interactions with other there were no medicinal products.

    Brimonidine is contraindicated in patients taking monoamine oxidase (MAO) inhibitors and in patients taking tricyclic or tetracyclic antidepressants (incl. mianserin).

    Brimonidine in a concentration of 2 mg / ml can enhance the effect of substances,affecting the central nervous system (alcohol, barbiturates, opioids, sedatives or anesthetics).

    Caution should be exercised in the case of drugs that can affect the absorption into the blood and metabolism of adrenaline, norepinephrine and other so-called biogenic amines (chlorpromazine, methylphenidate, reserpine).

    In some patients, after a brimonidine solution at a concentration of 2 mg / ml, there is a slight decrease in blood pressure. Caution should be exercised when using a combination of cardiac glycosides with hypotensive drugs and / or drugs.

    With simultaneous systemic administration of agonists or antagonists of adrenoreceptors (for example, isoprenaline or prazosin) for the first time, as well as changing the dose of these simultaneously administered systemic preparations (regardless of the mode of administration), interactions with alpha-adrenergic agonists or effects on their effects may occur .

    Special instructions:

    Avoid getting the drug on soft contact lenses, as it may discolour the latter. Before using the drug, contact lenses should be removed.The time interval between use of the drug and the re-installation of contact lenses should be at least 15 minutes.

    Do not use the solution after the expiry date indicated on the vial.

    Effect on the ability to drive transp. cf. and fur:

    The drug can cause fatigue or drowsiness, reduced vision, so during drug treatment should refrain from driving vehicles and servicing moving mechanisms.

    Form release / dosage:
    Eye drops 0.2%.
    Packaging:

    5 ml in bottles of white color from low-density polyethylene with a transparent drip-nozzle made of low-density polyethylene and a white screw cap made of high-density polyethylene with control of the first opening. A label is attached to the vial. 1 bottle together with the instruction for use is placed in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after the expiration date.

    Shelf life after opening the bottle is 4 weeks.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001434
    Date of registration:16.01.2012 / 14.02.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:VALEANT, LLC VALEANT, LLC Russia
    Manufacturer: & nbsp
    Santonika, UAB Lithuania
    Information update date: & nbsp08.01.2018
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